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https://www.readbyqxmd.com/read/29773502/design-synthesis-and-biological-evaluation-of-novel-pyrimidinedione-derivatives-as-dpp-4-inhibitors
#1
Ning Li, Li-Jun Wang, Bo Jiang, Shu-Ju Guo, Xiang-Qian Li, Xue-Chun Chen, Jiao Luo, Chao Li, Yi Wang, Da-Yong Shi
A series of novel pyrimidinedione derivatives were designed and evaluated for in vitro dipeptidyl peptidase-4 (DPP-4) inhibitory activity and in vivo anti-hyperglycemic efficacy. Among them, the representative compounds 11, 15 and 16 showed excellent inhibitory activity of DPP-4 with IC50 values of 64.47 nM, 188.7 nM and 65.36 nM, respectively. Further studies revealed that compound 11 was potent in vivo hypoglycemic effect. The structure-activity relationships of these pyrimidinedione derivatives had been discussed, which would be useful for developing novel DPP-4 inhibitors as treating type 2 diabetes...
May 14, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29769061/five-traditional-nigerian-polyherbal-remedies-protect-against-high-fructose-fed-streptozotocin-induced-type-2-diabetes-in-male-wistar-rats
#2
O E Kale, O B Akinpelu, A A Bakare, F O Yusuf, R Gomba, D C Araka, T O Ogundare, A C Okolie, O Adebawo, O Odutola
BACKGROUND: This present study sought to assess the modulatory effects of five Nigerian traditional polyherbal in high fructose-fed, streptozotocin-induced (HF-STZ) Type 2 diabetes (T2D) in rats. T2D was achieved via fructose feeding (20%W/V ) ad libitum for 2 weeks and streptozotocin (STZ, 40 mg/kg) (15th Day) intraperitoneally. METHODS: Seventy-two hours after STZ injection, fourty-eight diabetic rats were divided into eight of 6 rats/group: Diabetic normal untreated, glibenclamide (GBLI, 0...
May 16, 2018: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/29763691/insights-on-the-age-dependent-neurodegeneration-induced-by-monocrotophos-an-organophosphorous-insecticide-in-caenorhabditis-elegans-fed-high-glucose-evidence-in-wild-and-transgenic-strains
#3
Chinnu Salim, Nidheesh Thadathil, M Muralidhara, P S Rajini
The higher susceptibility of high glucose fed C. elegans to Monocrotophos (MCP, an organophosphorus insecticide) - induced dopaminergic (DA) neuronal degeneration was recently demonstrated. Employing this acute exposure model, the impact of MCP on DA degeneration among worms of two age groups (8 and 13 d old) fed control (CO) and high glucose (GF) diet with specific focus on phenotypic alterations, oxidative impairments and associated molecular perturbations employing both wild (N2) and transgenic strains(BZ555 and NL5901) was investigated...
May 12, 2018: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/29762637/set8-is-involved-in-the-regulation-of-hyperglycemic-memory-in-human-umbilical-endothelial-cells
#4
Xiangyuan Chen, Qichao Wu, Hui Jiang, Jiaqiang Wang, Yanjun Zhao, Yajun Xu, Minmin Zhu
Hyperglycemic memory occurs in diabetic cardiovascular complications, but the underlying mechanism remains to be elucidated. Although the depletion of SET8 leads to increased mitochondrial oxidative stress via increasing cellular reactive oxygen species (ROS) production, the role of SET8 in hyperglycemic memory-induced mitochondrial dysfunction is not well understood. Here, we investigated the role of SET8 in this setting. Our results showed that high glucose-induced vascular inflammation, ROS production and apoptosis remained at high levels even when glucose returned to normal level...
May 14, 2018: Acta Biochimica et Biophysica Sinica
https://www.readbyqxmd.com/read/29760953/hyperglycemia-potentiates-a-shift-from-apoptosis-to-rip1-dependent-necroptosis
#5
William D McCaig, Payal S Patel, Sergey A Sosunov, Nicole L Shakerley, Tori A Smiraglia, Miranda M Craft, Katharine M Walker, Matthew A Deragon, Vadim S Ten, Timothy J LaRocca
Apoptosis and necroptosis are the primary modes of eukaryotic cell death, with apoptosis being non-inflammatory while necroptosis is highly inflammatory. We previously demonstrated that, once activated, necroptosis is enhanced by hyperglycemia in several cell types. Here, we determine if hyperglycemia affects apoptosis similarly. We show that hyperglycemia does not enhance extrinsic apoptosis but potentiates a shift to RIP1-dependent necroptosis. This is due to increased levels and activity of RIP1, RIP3, and MLKL, as well as decreased levels and activity of executioner caspases under hyperglycemic conditions following stimulation of apoptosis...
2018: Cell Death Discovery
https://www.readbyqxmd.com/read/29760374/overview-of-cerebral-edema-during-correction-of-hyperglycemic-crises
#6
Daniel Varela, Natalie Held, Stuart Linas
BACKGROUND Hyperglycemic crises can cause severe neurologic impairment. One of the most dreaded consequences of hyperglycemic crises is cerebral edema, a rare complication seen during the treatment of hyperglycemic crises resulting from overly-aggressive fluid resuscitation and rapid correction of hyperglycemia and hyperosmolarity. CASE REPORT We present a case of profound hyperglycemic crisis with blood glucose greater than 2000 mg/dL, complicated by the development of new neurologic deficits after rapid correction of hyperglycemia...
May 15, 2018: American Journal of Case Reports
https://www.readbyqxmd.com/read/29757412/development-of-a-provincial-initiative-to-improve-glucose-control-in-critically-ill-patients
#7
Peter Dodek, Shari McKeown, Eric Young, Vinay Dhingra
Objective: To describe the development, implementation and initial evaluation of an initiative to improve glucose control in critically ill patients. Design: Glucose control in critically ill patients was chosen by critical care leaders as a target for improvement. This was an observational study to document changes in processes and measures of glucose control in each intensive care unit (ICU). ICU nurse educators were interviewed to document relevant changes between April 2012 and April 2016...
May 11, 2018: International Journal for Quality in Health Care
https://www.readbyqxmd.com/read/29756477/anti-hyperglycemic-and-anti-inflammatory-activities-of-polyphenolic-rich-extract-of-syzygium-cumini-linn-leaves-in-alloxan-induced-diabetic-rats
#8
Basiru O Ajiboye, Oluwafemi A Ojo, Olivia S Akuboh, Okesola M Abiola, Olajumoke Idowu, Aliyu O Amuzat
In this study, anti-hyperglycemic and anti-inflammatory activities of polyphenolic-rich extract of Syzygium cumini leaves in alloxan-induced diabetic rats were determined. Diabetes was induced by a single intraperitoneal injection of alloxan (150 mg/kg body weight) in female Wistar rats. The rats were orally administered with 400 mg/kg free phenol, 400 mg/kg bound phenol, and 5 mg/kg metformin, respectively. On the 14th day of oral administration, the animals were sacrificed, anti-hyperglycemic and anti-inflammatory were assessed...
January 2018: Journal of evidence-based integrative medicine
https://www.readbyqxmd.com/read/29753610/improvement-of-hyperglycemia-in-a-murine-model-of-insulin-resistance-and-high-glucose-and-inflammasome-mediated-il-1%C3%AE-expressions-in-macrophages-by-silymarin
#9
Chun-Ping Lu, Chien-Yu Huang, Szu-Hsuan Wang, Chih-Hsien Chiu, Lan-Hui Li, Kuo-Feng Hua, Tzu-Hua Wu
Macrophages and inflammasome pathway are involved in high-glucose toxicity and development of insulin resistance. Silymarin (SMR) was known to modulate glucose homeostasis and reduce inflammation. However, it is still unknown whether SMR possess anti-hyperglycemic effects in diabetic-like knockout mice (Hnf-1αkin/- /Ins.cre mice) with insulin resistance and also unclear how SMR regulates LPS induced stress markers and pro-inflammatory cytokines under stresses of high glucose (HG) or NLRP3 inflammasome activation...
May 10, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29751356/exploring-novel-pharmacotherapeutic-applications-and-repurposing-potential-of-sodium-glucose-cotransporter-2-sglt2-inhibitors
#10
REVIEW
Tushar Madaan, Ibraheem Husain, Mohamad Akhtar, Abul Kalam Najmi
Sodium glucose cotransporter 2 (SGLT2) inhibitors are a relatively new class of anti-hyperglycemic drugs with a distinctive mechanism of action focusing on renal absorption ofglucose. Apart from its anti-hyperglycemic effects, a multitude of research studies on this classhave revealed that these drugs have far more versatile and comprehensive pharmacologicaleffects than previously believed. Approximately 30% of FDA approved drugs are repurposedand used for indications other than those they were initially intended for...
May 11, 2018: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/29750990/streptozotocin-induced-hyperglycemia-stimulates-molecular-signaling-that-promotes-cell-cycle-reentry-in-mouse-hippocampus
#11
Euitaek Yang, Kartheek Gavini, Ami Bhakta, Muralikrishnan Dhanasekaran, Izhar Khan, Kodeeswaran Parameshwaran
AIMS: Cerebral atrophy resulting from neurodegeneration is highly prevalent in individuals with diabetes; however, the underlying mechanisms for diabetic neurodegeneration are not fully understood. Here we hypothesized that hyperglycemia induces molecular signaling that favors induction of proliferation in post mitotic, fully differentiated hippocampal neurons. MATERIALS AND METHODS: Streptozotocin (150 mg/kg) was intraperitoneally injected to four months old male mice to induce diabetes...
May 8, 2018: Life Sciences
https://www.readbyqxmd.com/read/29750969/tissue-distribution-and-biochemical-characteristics-of-receptors-for-sinus-gland-peptide-vii-as-a-crustacean-hyperglycemic-hormone-and-vitellogenesis-inhibiting-hormone-of-the-kuruma-prawn-marsupenaeus-japonicus
#12
Chiaki Nagai-Okatani, Shinji Nagata, Hiromichi Nagasawa
Crustacean hyperglycemic hormone (CHH) and vitellogenesis-inhibiting hormone (VIH) belong to the CHH family, a neuropeptide superfamily conserved in ecdysozoans. To date, no receptor for the CHH family peptides has been identified in crustaceans. Here, we used a CHH family isoform, Mj-sinus gland peptide (SGP) -VII, as a representative of CHH and VIH in order to determine its target tissues and obtain biochemical information regarding its receptor in the kuruma prawn Marsupenaeus japonicus (Crustacea, Decapoda)...
May 8, 2018: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/29750414/glucose-dependent-insulinotropic-polypeptide-increases-blood-flow-in-adipose-tissue-of-humans-by-recruiting-capillaries
#13
Meena Asmar, Ali Asmar, Lene Simonsen, Jens Juul Holst, Jens Bülow
Context and objektive: Glucose-dependent insulinotropic polypeptide (GIP) in combination with hyperinsulinemia increase blood flow and triglyceride clearance in subcutaneous abdominal adipose tissue in lean humans. The present experiments were performed to determine whether the increase may involve capillary recruitment. Design: Eight lean healthy volunteers were studied before and after 1-h infusion of GIP or saline during a hyperglycemic-hyperinsulinemic clamp, raising plasma glucose and insulin to postprandial levels...
May 9, 2018: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29750032/protection-of-silver-nanoparticles-using-eysenhardtia-polystachya-in-peroxide-induced-pancreatic-%C3%AE-cell-damage-and-their-antidiabetic-properties-in-zebrafish
#14
Abraham Heriberto Garcia Campoy, Rosa Martha Perez Gutierrez, Gabriela Manriquez-Alvirde, Alethia Muñiz Ramirez
Background: The aim was to explore the efficacy of extract of Eysenhardtia polystachya -loaded silver nanoparticles (EP/AgNPs) on pancreatic β cells, INS-1 cells, and zebrafish as a valuable model for the study of diabetes mellitus. Materials and methods: EP/AgNPs were synthesized using methanol/water bark extract of E. polystachya and characterized using various physicochemical techniques. Results: Immersion of adult zebrafish in 111 mM glucose solution resulted in a sustained hyperglycemic, hyperlipidemic state, and serum insulin levels decreased...
2018: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29749986/-urtica-dioica-distillate-regenerates-pancreatic-beta-cells-in-streptozotocin-induced-diabetic-rats
#15
Ali Gohari, Ali Noorafshan, Masoumeh Akmali, Fahimeh Zamani-Garmsiri, Atefeh Seghatoleslam
Background: Urtica dioica is known as an anti-hyperglycemic plant. Urtica dioica distillate (UD) is a traditional Iranian drink, locally known as "aragh gazaneh". In spite of its widespread consumption in Iran, according to traditional Iranian medicine, there is no scientific report on the usefulness of UD for diabetic patients. This survey was designed to evaluate its protective effects for the recovery from diabetes by determining the serum insulin, blood glucose, volume of pancreatic islets, and the number and volume of β-cells in diabetic rats...
March 2018: Iranian Journal of Medical Sciences
https://www.readbyqxmd.com/read/29749643/insulin-dysregulation-in-horses-with-systemic-inflammatory-response-syndrome
#16
François-René Bertin, Debra Ruffin-Taylor, Allison Jean Stewart
BACKGROUND: Systemic inflammation is a cause of insulin dysregulation in many species, but the insulin and glucose dynamics in adult horses diagnosed with systemic inflammatory response syndrome (SIRS) are poorly documented. HYPOTHESIS/OBJECTIVES: In SIRS in horses, insulin and glucose dynamics will be altered and associated with survival. ANIMALS: Adult horses diagnosed with SIRS admitted to a referral hospital. METHODS: Prospective study enrolling horses diagnosed with SIRS in which serum insulin and glucose concentrations were measured...
May 10, 2018: Journal of Veterinary Internal Medicine
https://www.readbyqxmd.com/read/29746846/o-linked-n-acetyl-glucosamine-deposition-in-placental-proteins-varies-according-to-maternal-glycemic-levels
#17
Vanessa Dela Justina, Rinaldo R Dos Passos Junior, Alecsander F Bressan, Rita C Tostes, Fernando S Carneiro, Thaigra S Soares, Gustavo T Volpato, Victor Vitorino Lima, Sebastian San Martin, Fernanda R Giachini
AIMS: Hyperglycemia increases glycosylation with O-linked N‑acetyl‑glucosamine (O-GlcNAc) contributing to placental dysfunction and fetal growth impairment. Our aim was to determine how O-GlcNAc levels are affected by hyperglycemia and the O-GlcNAc distribution in different placental regions. MAIN METHODS: Female Wistar rats were divided into the following groups: severe hyperglycemia (>300 mg/dL; n = 5); mild hyperglycemia (>140 mg/dL, at least than two time points during oral glucose tolerance test; n = 7) or normoglycemia (<120 mg/dL; n = 6)...
May 7, 2018: Life Sciences
https://www.readbyqxmd.com/read/29745916/fournier-s-gangrene-a-rare-complication-of-diabetes-mellitus-case-report
#18
Sh Muharremi
The presented case reports on 54-years old patient with T2 Diabetes mellitus who, due to hypoglycemic episodes on Insulin therapy, was treated with oral anti-hyperglycemic medications. Patient was on hemodialysis due to the stage 5 chronic kidney failure and had various comorbid conditions: arterial hypertension, history of acute myocardial infarction, dilative cardiomyopathy, amaurosis and peripheral neuropathy. Besides his complicated medical history, patient developed an early stage of Fournier's gangrene...
April 2018: Georgian Medical News
https://www.readbyqxmd.com/read/29743758/the-impact-of-dopamine-on-insulin-secretion-in-healthy-controls
#19
Lisa J Underland, Erika R Mark, Ranjitha Katikaneni, Rubina Heptulla
Objective: Dopamine is very commonly used in the critical care setting and impacts glucose homeostasis. In some studies, it is noted to increase insulin resistance or decrease insulin secretion. The role of insulin secretion in response to dopamine is incompletely understood. Methods: Eight individuals underwent a hyperglycemic clamp with a dopamine infusion, and eight controls underwent hyperglycemic clamp alone. Insulin, C-peptide, glucagon, cortisol, and norepinephrine (NE) concentrations were measured at various time points...
April 2018: Indian Journal of Critical Care Medicine
https://www.readbyqxmd.com/read/29739273/angiogenic-dysregulation-in-pregnancy-related-hypertension-a-role-for-metformin
#20
Nerolen Soobryan, Saravanakumar Murugesan, Arunagiri Pandiyan, Jagidesa Moodley, Irene Mackraj
In the face of escalating maternal and fetal health threats, hypertensive pregnancy disorders (HPDs) is one of the leading cause of maternal and fetal morbidity and mortality. The range of HPDs include white-coat hypertension, chronic hypertension, gestational hypertension, mild-to-moderate and severe preeclampsia and eclampsia. Current evidence implicates an imbalance of circulating anti- and angiogenic factors in HPDs emanating from the placental vasculature, impacting on angiogenesis. Delivery of the fetus is thus far the only curative measure, albeit with increased risk...
January 1, 2018: Reproductive Sciences
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